ERbeta ligands. Part 4: Synthesis and structure-activity relationships of a series of 2-phenylquinoline derivatives.

Article Details

Citation
Copy to clipboard

Vu AT, Cohn ST, Manas ES, Harris HA, Mewshaw RE

ERbeta ligands. Part 4: Synthesis and structure-activity relationships of a series of 2-phenylquinoline derivatives.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4520-5.

PubMed ID
16098741 [ View in PubMed
]
Abstract

A new class of estrogen receptor beta (ERbeta) ligands based on the 2-phenylquinoline scaffold was prepared. Several analogues with C4 substitution displayed high affinity (3-5 nM) and significant selectivity (up to 83-fold) for ERbeta. The best compound, 13b, was profiled as a selective partial agonist for ERbeta at 1 muM in a cell-based transcriptional assay. Uterine weight bioassay of 13b indicated no activation of ERalpha in vivo.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
EstradiolEstrogen receptor alphaIC 50 (nM)3.2N/AN/ADetails
EstradiolEstrogen receptor betaIC 50 (nM)3.6N/AN/ADetails
GenisteinEstrogen receptor alphaIC 50 (nM)395N/AN/ADetails
GenisteinEstrogen receptor betaIC 50 (nM)10N/AN/ADetails